Glesatinib: Difference between revisions

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{{Infobox drug
{{DISPLAYTITLE:Glesatinib}}
| IUPAC_name        = ''N''-[(3-Fluoro-4-<nowiki/>{[2-(5-<nowiki/>{[(2-methoxyethyl)amino]methyl}-2-pyridinyl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)carbamothioyl]-2-(4-fluorophenyl)acetamide
| image            = Glesatinib skeletal.svg
| alt              =
| caption          =
<!-- Clinical data -->
| pronounce        =
| tradename        =
| Drugs.com        =
| MedlinePlus      =
| pregnancy_AU      = <!-- A/B1/B2/B3/C/D/X -->
| pregnancy_AU_comment =
| pregnancy_US      = <!-- A/B/C/D/X/N -->
| pregnancy_category=
| routes_of_administration = [[Oral administration|By mouth]]
| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled-->
| legal_AU_comment =
| legal_CA = <!-- OTC, Rx-only, Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_DE = <!-- Anlage I, II, III -->
| legal_NZ = <!-- Class A, B, C -->
| legal_UK = <!-- GSL, P, POM, CD, CD Lic, CD POM, CD No Reg POM, CD (Benz) POM, CD (Anab) POM or CD Inv POM / Class A, B, C -->
| legal_US = <!-- OTC/Rx-only/Schedule I, II, III, IV, V -->
| legal_UN = <!-- N I, II, III, IV / P I, II, III, IV-->
| legal_status      = Investigational
<!-- Pharmacokinetic data -->
| bioavailability  =
| protein_bound    =
| metabolism        =
| metabolites      =
| onset            =
| elimination_half-life =
| duration_of_action =
| excretion        =
<!-- Identifiers -->
| CAS_number        = 936694-12-1
| class            =
| ATCvet            =
| ATC_prefix        = None
| ATC_suffix        =
| PubChem          = 25181472
| DrugBank          =
| ChemSpiderID      = 52084900
| UNII              = 7Q29OXD98N
| KEGG = D11136
<!-- Chemical and physical data -->
| chemical_formula  =
| C=31 | H=27 | F=2 | N=5 | O=3 | S=2
| molecular_weight  =
| smiles = COCCNCc1ccc(nc1)c2cc3c(s2)c(ccn3)Oc4ccc(cc4F)NC(=S)NC(=O)Cc5ccc(cc5)F
| StdInChI=1S/C31H27F2N5O3S2/c1-40-13-12-34-17-20-4-8-24(36-18-20)28-16-25-30(43-28)27(10-11-35-25)41-26-9-7-22(15-23(26)33)37-31(42)38-29(39)14-19-2-5-21(32)6-3-19/h2-11,15-16,18,34H,12-14,17H2,1H3,(H2,37,38,39,42)
| StdInChIKey = YRCHYHRCBXNYNU-UHFFFAOYSA-N
}}


'''Glesatinib''' ('''MGCD265''') is an experimental anti-cancer drug.<ref name=cg>[https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=597305 glesatinib@cancer.gov]</ref>
== Overview ==
'''Glesatinib''' is a small molecule [[tyrosine kinase inhibitor]] that is being investigated for its potential use in the treatment of various types of [[cancer]]. It specifically targets the [[MET]] receptor tyrosine kinase, which is often overexpressed or mutated in certain cancer types, leading to uncontrolled cell growth and proliferation.


It is in phase 2 clinical trials for [[non-small cell lung cancer]] (NSCLC).<ref name=ct991>[https://clinicaltrials.gov/ct2/show/NCT02954991 Phase 2 Study of Glesatinib, Sitravatinib or Mocetinostat in Combination With Nivolumab in Non-Small Cell Lung Cancer]</ref>
== Mechanism of Action ==
Glesatinib works by inhibiting the activity of the MET receptor. The MET receptor is a [[proto-oncogene]] that, when activated, can trigger a cascade of downstream signaling pathways involved in cell growth, survival, and metastasis. By blocking MET, glesatinib aims to halt the progression of cancer by preventing these signals from being transmitted.


It is a spectrum selective tyrosine<ref name=cg/> [[kinase inhibitor]] "for the treatment of non-small cell lung cancer (NSCLC) patients with genetic alterations of [[C-Met|MET]]".<ref>[http://pipelinereview.com/index.php/2017010663534/Small-Molecules/Mirati-Therapeutics-Provides-Update-On-Glesatinib-And-Sitravatinib-Clinical-Trials-And-Pipeline-Programs.html Mirati Therapeutics Provides Update On Glesatinib And Sitravatinib Clinical Trials And Pipeline Programs. Jan 2017]</ref>
[[File:Glesatinib_skeletal.svg|thumb|right|Chemical structure of Glesatinib]]


==References==
== Clinical Development ==
{{reflist}}
Glesatinib is currently undergoing clinical trials to evaluate its efficacy and safety in patients with MET-positive cancers. These trials are crucial for determining the appropriate dosing, potential side effects, and overall therapeutic benefit of the drug.


==External links==
== Potential Indications ==
*[https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=597305 glesatinib@cancer.gov]
The primary focus of glesatinib research is on [[non-small cell lung cancer]] (NSCLC) and other solid tumors that exhibit MET dysregulation. Researchers are also exploring its use in combination with other therapies to enhance its anticancer effects.


[[Category:Tyrosine kinase inhibitors]]
== Side Effects ==
[[Category:Acetamides]]
As with many targeted therapies, glesatinib may cause a range of side effects. Commonly reported side effects include fatigue, nausea, and diarrhea. More serious adverse effects may occur, necessitating close monitoring of patients during treatment.
[[Category:Thioureas]]
 
[[Category:Fluoroarenes]]
== Future Directions ==
[[Category:Experimental cancer drugs]]
Ongoing research aims to better understand the role of MET in cancer and to identify biomarkers that can predict response to glesatinib. This will help in personalizing treatment plans and improving outcomes for patients.


== Related Pages ==
* [[Tyrosine kinase inhibitor]]
* [[MET receptor]]
* [[Non-small cell lung cancer]]
* [[Cancer treatment]]


{{antineoplastic-drug-stub}}
[[Category:Antineoplastic drugs]]
{{dictionary-stub1}}
[[Category:Tyrosine kinase inhibitors]]

Latest revision as of 11:34, 15 February 2025


Overview[edit]

Glesatinib is a small molecule tyrosine kinase inhibitor that is being investigated for its potential use in the treatment of various types of cancer. It specifically targets the MET receptor tyrosine kinase, which is often overexpressed or mutated in certain cancer types, leading to uncontrolled cell growth and proliferation.

Mechanism of Action[edit]

Glesatinib works by inhibiting the activity of the MET receptor. The MET receptor is a proto-oncogene that, when activated, can trigger a cascade of downstream signaling pathways involved in cell growth, survival, and metastasis. By blocking MET, glesatinib aims to halt the progression of cancer by preventing these signals from being transmitted.

File:Glesatinib skeletal.svg
Chemical structure of Glesatinib

Clinical Development[edit]

Glesatinib is currently undergoing clinical trials to evaluate its efficacy and safety in patients with MET-positive cancers. These trials are crucial for determining the appropriate dosing, potential side effects, and overall therapeutic benefit of the drug.

Potential Indications[edit]

The primary focus of glesatinib research is on non-small cell lung cancer (NSCLC) and other solid tumors that exhibit MET dysregulation. Researchers are also exploring its use in combination with other therapies to enhance its anticancer effects.

Side Effects[edit]

As with many targeted therapies, glesatinib may cause a range of side effects. Commonly reported side effects include fatigue, nausea, and diarrhea. More serious adverse effects may occur, necessitating close monitoring of patients during treatment.

Future Directions[edit]

Ongoing research aims to better understand the role of MET in cancer and to identify biomarkers that can predict response to glesatinib. This will help in personalizing treatment plans and improving outcomes for patients.

Related Pages[edit]

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